Bergstrom C P, Clarke R, Fitzloff J F, Lu M C
Department of Medicinal Chemistry and Pharmacognosy, College of Pharmacy, University of Illinois, Chicago 60612.
Drug Des Deliv. 1991 Jul;7(4):259-68.
Three 22-(p-chloroaryl) analogues of cholesterol (6a-c) were synthesized and evaluated as potential inhibitors of the adrenal cholesterol side-chain cleavage enzyme, in comparison with the known 20-aryl analogue, 20-(p-chlorophenyl)-5-prenen-3 beta,20-diol (2b). All were potent inhibitors. An oxygen at C-22 (analogues 6a and 6b) enhanced the strong binding to the enzyme. Two compounds (6b and 6c) are potential substrates of the enzyme. Possible pharmaceutical uses for these compounds and their derivatives are discussed.
合成了三种胆固醇的22 - （对氯芳基）类似物（6a - c），并将其作为肾上腺胆固醇侧链裂解酶的潜在抑制剂进行评估，同时与已知的20 - 芳基类似物20 - （对氯苯基）-5 - 异戊二烯 - 3β，20 - 二醇（2b）进行比较。所有这些都是强效抑制剂。C - 22位的氧（类似物6a和6b）增强了与该酶的强结合。两种化合物（6b和6c）是该酶的潜在底物。讨论了这些化合物及其衍生物可能的药用用途。
